talwin
Generic Name: (
Pentazocine Lactate)
Dosage Type: injection, solution Organization: Hospira, Inc.
CIV
Analgesic
for Parenteral Use
Rx only
DESCRIPTION
TALWIN injection, Pentazocine Lactate Injection, USP, is
a member of the benzazocine series (also known as the benzomorphan series).
Chemically, pentazocine lactate is 1, 2, 3, 4, 5, 6-hexahydro-6,11-dimethyl-3-(3-methyl-2-butenyl)-2,6-methano-3-benzazocin-8-ol
lactate, a white, crystalline substance soluble in acidic aqueous solutions.
CLINICAL PHARMACOLOGY
TALWIN is a potent analgesic and 30 mg is usually as effective
an analgesic as morphine 10 mg or meperidine 75 mg to 100 mg; however, a few
studies suggest the TALWIN to morphine ratio may range from 20 mg to 40 mg
TALWIN to 10 mg morphine. The duration of analgesia may sometimes be less
than that of morphine. Analgesia usually occurs within 15 to 20 minutes after
intramuscular or subcutaneous injection and within 2 to 3 minutes after intravenous
injection. TALWIN weakly antagonizes the analgesic effects of morphine, meperidine,
and phenazocine; in addition, it produces incomplete reversal of cardiovascular,
respiratory, and behavioral depression induced by morphine and meperidine.
TALWIN has about 1/50 the antagonistic activity of nalorphine. It also has
sedative activity.
Clinical data indicate that differences
in various pharmacokinetic parameters may be observed with increasing age.
In one study, elderly patients exhibited a longer mean elimination half-life,
a lower mean total plasma clearance, and a larger mean area under the concentration-time
curve than younger patients.
INDICATIONS AND USAGE
For the relief of moderate to severe pain. TALWIN may also
be used for preoperative or preanesthetic medication and as a supplement to
surgical anesthesia.
CONTRAINDICATION
TALWIN should not be administered to patients who are hypersensitive
to it.
WARNINGS
Drug Dependence:Special care should be exercised in prescribing pentazocine
for emotionally unstable patients and for those with a history of drug misuse.
Such patients should be closely supervised when greater than 4 or 5 days of
therapy is contemplated. There have been instances of psychological and physical
dependence on TALWIN in patients with such a history and, rarely, in patients
without such a history. Extended use of parenteral TALWIN may lead to physical
or psychological dependence in some patients. When TALWIN is abruptly discontinued,
withdrawal symptoms such as abdominal cramps, elevated temperature, rhinorrhea,
restlessness, anxiety, and lacrimation may occur. However, even when these
have occurred, discontinuance has been accomplished with minimal difficulty.
In the rare patient in whom more than minor difficulty has been encountered,
reinstitution of parenteral TALWIN with gradual withdrawal has ameliorated
the patient’s symptoms. Substituting methadone or other narcotics for
TALWIN in the treatment of the pentazocine abstinence syndrome should be avoided.
There have been rare reports of possible abstinence syndromes in newborns
after prolonged use of TALWIN during pregnancy.
In prescribing parenteral TALWIN for chronic use, particularly
if the drug is to be self-administered, the physician should take precautions
to avoid increases in dose and frequency of injection by the patient.
Just as with all medication, the oral form of TALWIN is
preferable for chronic administration.
Tissue Damage at Injection Sites: Severe sclerosis
of the skin, subcutaneous tissues, and underlying muscle have occurred at
the injection sites of patients who have received multiple doses of pentazocine
lactate. Constant rotation of injection sites is, therefore, essential. In
addition, animal studies have demonstrated that TALWIN is tolerated less well
subcutaneously than intramuscularly. (See DOSAGE
AND ADMINISTRATION.)
Head
Injury and Increased Intracranial Pressure: As in the case of other
potent analgesics, the potential of TALWIN injection for elevating cerebrospinal
fluid pressure may be attributed to CO2 retention due to the respiratory
depressant effects of the drug. These effects may be markedly exaggerated
in the presence of head injury, other intracranial lesions, or a preexisting
increase in intracranial pressure. Furthermore, TALWIN can produce effects
which may obscure the clinical course of patients with head injuries. In such
patients, TALWIN must be used with extreme caution and only if its use is
deemed essential.
Acute CNS
Manifestations: Patients receiving therapeutic doses of pentazocinehave experienced hallucinations (usually visual), disorientation, and confusion
which have cleared spontaneously within a period of hours. The mechanism of
this reaction is not known. Such patients should be closely observed and vital
signs checked. If the drug is reinstituted, it should be done with caution
since these acute CNS manifestations may recur.
Due
to the potential for increased CNS depressant effects, alcohol should be used
with caution in patients who are currently receiving pentazocine.
Ambulatory Patients: Since sedation, dizziness,
and occasional euphoria have been noted, ambulatory patients should be warned
not to operate machinery, drive cars, or unnecessarily expose themselves to
hazards.
Myocardial Infarction: Caution should be exercised in the intravenous use of pentazocine
for patients with acute myocardial infarction accompanied by hypertension
or left ventricular failure. Data suggest that intravenous administration
of pentazocine increases systemic and pulmonary arterial pressure and systemic
vascular resistance in patients with acute myocardial infarction.
NOTE: Acetone sodium bisulfite, a sulfite that
may cause allergic-type reactions including anaphylactic symptoms and life-threatening
or less severe asthmatic episodes in certain susceptible people, is contained
in both Carpuject® Sterile Cartridge Units and multiple-dose
vials. The overall prevalence of sulfite sensitivity in the general population
is unknown and probably low. Sulfite sensitivity is seen more frequently in
asthmatic than in nonasthmatic people.
The ampuls in
the Uni-Amp® Pak do not contain acetone sodium bisulfite.
PRECAUTIONS
Certain Respiratory Conditions: The possibility that TALWIN may cause respiratory depression should
be considered in treatment of patients with bronchial asthma. TALWIN should
be administered only with caution and in low dosage to patients with respiratory
depression (e.g., from other medication, uremia, or severe infection), severely
limited respiratory reserve, obstructive respiratory conditions, or cyanosis.
Impaired Renal or Hepatic Function: Although laboratory
tests have not indicated that TALWIN causes or increases renal or hepatic
impairment, the drug should be administered with caution to patients with
such impairment. Extensive liver disease appears to predispose to greater
side effects (e.g., marked apprehension, anxiety, dizziness, sleepiness) from
the usual clinical dose, and may be the result of decreased metabolism of
the drug by the liver.
Biliary
Surgery: Narcotic drug products are generally considered to elevate
biliary tract pressure for varying periods following their administration.
Some evidence suggests that pentazocine may differ from other marketed narcotics
in this respect (i.e., it causes little or no elevation in biliary tract pressures).
The clinical significance of these findings, however, is not yet known.
Patients Receiving Narcotics: TALWIN is a mild
narcotic antagonist. Some patients previously given narcotics, including methadone
for the daily treatment of narcotic dependence, have experienced withdrawal
symptoms after receiving TALWIN.
CNS
Effect: Caution should be used when TALWIN is administered to patients
prone to seizures; seizures have occurred in a few such patients in association
with the use of TALWIN although no cause and effect relationship has been
established.
Use in Anesthesia: Concomitant use of CNS depressants with parenteral TALWIN may
produce additive CNS depression. Adequate equipment and facilities should
be available to identify and treat systemic emergencies should they occur.
Usage in Pregnancy:
Safe use of TALWIN during pregnancy (other than labor) has
not been established. Animal reproduction studies have not demonstrated teratogenic
or embryotoxic effects. However, TALWIN should be administered to pregnant
patients (other than labor) only when, in the judgment of the physician, the
potential benefits outweigh the possible hazards. Patients receiving TALWIN
during labor have experienced no adverse effects other than those that occur
with commonly used analgesics. TALWIN should be used with caution in women
delivering premature infants.
Pediatric Use:
The safety and efficacy of TALWIN as preoperative or preanesthetic
medication have been established in pediatric patients 1 to16 years of age.
Use of TALWIN in these age groups is supported by evidence from adequate and
controlled studies in adults with additional data from published controlled
trials in pediatric patients. The safety and efficacy of TALWIN as a premedication
for sedation have not been established in pediatric patients less than one
year old. Information on the safety profile of TALWIN as a postoperative analgesic
in children less than 16 years is limited.
Geriatric Use:
Elderly patients may be more sensitive to the analgesic effects
of TALWIN than younger patients. (See DOSAGE
AND ADMINISTRATION.)
Clinical data indicate
that differences in various pharmacokinetic parameters of TALWIN may exist
between elderly and younger patients. (See CLINICAL
PHARMACOLOGY.)
Sedating drugs may cause confusion
and oversedation in the elderly; elderly patients generally should be started
on low doses of TALWIN and observed closely.
This drug
is known to be substantially excreted by the kidney, and the risk of toxic
reactions to this drug may be greater in patients with impaired renal function.
Because elderly patients are more likely to have decreased renal function,
care should be taken in dose selection, and it may be useful to monitor renal
function.
ADVERSE REACTIONS
The most commonly occurring reactions are: nausea, dizziness
or lightheadedness, vomiting, euphoria.
Dermatologic
Reactions: Soft tissue induration, nodules, and cutaneous depression
can occur at injection sites. Ulceration (sloughing) and severe sclerosis
of the skin and subcutaneous tissues (and, rarely, underlying muscle) have
been reported after multiple doses. Other reported dermatologic reactions
include diaphoresis, sting on injection, flushed skin including plethora,
dermatitis including pruritus.
Infrequently occurring
reactions are—respiratory: respiratory
depression, dyspnea, transient apnea in a small number of newborn infants
whose mothers received TALWIN during labor; cardiovascular: circulatory depression, shock, hypertension; CNS
effects: dizziness, lightheadedness, hallucinations, sedation, euphoria,
headache, confusion, disorientation; infrequently weakness, disturbed dreams,
insomnia, syncope, visual blurring and focusing difficulty, depression; and
rarely tremor, irritability, excitement, tinnitus; gastrointestinal: constipation, dry mouth; other:
urinary retention, headache, paresthesia, alterations in rate or strength
of uterine contractions during labor.
Rarely reported
reactions include—neuromuscular and psychiatric: muscle tremor, insomnia, disorientation,
hallucinations; gastrointestinal: taste
alteration, diarrhea and cramps; ophthalmic:
blurred vision, nystagmus, diplopia, miosis; hematologic: depression of white blood cells (especially granulocytes), which
is usually reversible, moderate transient eosinophilia; other: tachycardia, weakness or faintness, chills; allergic reactions
including edema of the face, toxic epidermal necrolysis. (See Acute
CNS Manifestations and Drug Dependence under WARNINGS.)
DOSAGE AND ADMINISTRATION
Adults, Excluding Patients in Labor: The recommended single parenteral dose is 30 mg by intramuscular,
subcutaneous, or intravenous route. This may be repeated every 3 to 4 hours.
Doses in excess of 30 mg intravenously or 60 mg intramuscularly or subcutaneously
are not recommended. Total daily dosage should not exceed 360 mg. Elderly
patients may be more sensitive to the analgesic effects of TALWIN than younger
patients. Elderly patients generally should be started on low doses of TALWIN
and observed closely.
The subcutaneous route of administration
should be used only when necessary because of possible severe tissue damage
at injection sites (see WARNINGS).
When frequent injections are needed, the drug should be administered intramuscularly.
In addition, constant rotation of injection sites (e.g., the upper outer quadrants
of the buttocks, mid-lateral aspects of the thighs, and the deltoid areas)
is essential.
Patients in
Labor: A single, intramuscular 30 mg dose has been most commonly
administered. An intravenous 20 mg dose has given adequate pain relief to
some patients in labor when contractions become regular, and this dose may
be given two or three times at two- to three-hour intervals, as needed.
Pediatric Patients Excluding Patients Less Than One Year
Old: The recommended single parenteral dose as premedication for
sedation is 0.5 mg/kg by intramuscular route.
CAUTION: TALWIN should not be mixed in the same
syringe with soluble barbiturates because precipitation will occur.
OVERDOSAGE
Manifestations: Clinical
experience with TALWIN overdosage has been insufficient to define the signs
of this condition.
Treatment: Oxygen, intravenous fluids, vasopressors, and other supportive
measures should be employed as indicated. Assisted or controlled ventilation
should also be considered. For respiratory depression due to overdosage or
unusual sensitivity to TALWIN, parenteral naloxone is a specific and effective
antagonist.
HOW SUPPLIED
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List
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Container
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Concentration
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Fill
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Quantity
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1920
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Multiple-Dose Vial
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30 mg/mL
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10 mL
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Box of 10
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Each mL contains pentazocine lactate
equivalent to 30 mg base and 2 mg acetone sodium bisulfite, 1.5 mg sodium
chloride, and 1 mg methylparaben as preservative, in Water for Injection.
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1938
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Carpuject® (22-Gauge, 1/4”
needle)
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30 mg/mL
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2 mL
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Box of 10
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1938
|
Carpuject® (Luer Lock)
|
30 mg/mL
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2 mL
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Box of 10
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Each mL contains pentazocine lactate
equivalent to 30 mg base, 1 mg acetone sodium bisulfite, and 2.2 mg sodium
chloride, in Water for Injection.
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1941
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Ampul
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30 mg/mL
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1 mL
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Uni-Amp®
Pak
of 25
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Each mL contains pentazocine lactate
equivalent to 30 mg base and 2.8 mg sodium chloride, in Water for Injection.
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The pH of TALWIN solutions is adjusted between 4 and 5
with lactic acid or sodium hydroxide. The air in the ampuls, vials, and cartridge
units has been displaced by nitrogen gas.
Store at controlled
room temperature 15° to 30°C (59° to 86°F). [See USP.]
June, 2004
©Hospira 2004 EN-0253 Printed in USA
HOSPIRA, INC., LAKE FOREST, IL 60045 USA
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Revised: 10/2006Hospira, Inc.